Paracetamol/ naproxen co-crystals; a simple way for improvement of flowability, tableting and dissolution properties

Purpose: To develop glibenclamide-nicotinamide cocrystals with the solvent evaporation method and evaluate their solubility and dissolution properties. Methods: Cocrystals of glibenclamide-nicotinamide (1:2) were prepared with the solvent evaporation method. The prediction of interactive cocrystals was observed using in silico method. The solubility and dissolution were performed as evaluation of cocrystals. The cocrystals also were characterized by differential scanning calorimetry (DSC), infrared spectrophotometry, and powder X-ray diffraction (PXRD). Result: The solubility and dissolution profile of glibenclamide-nicotinamide cocrystal (1:2) increased significantly compared to pure glibenclamide as well as its physical mixture. Characterization of cocrystal glibenclamide-nicotinamide (1:2) including infrared Fourier transform, DSC, and PXRD, indicated the formation of a new solid crystal phase differing from glibenclamide and nicotinamide. Conclusion: The confirmation of cocrystal glibenclamide-nicotinamide (1:2) indicated the formation of new solid crystalline phases that differ from pure glibenclamide and its physical mixture

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Physicochemical Characterization of Solid Dispersions of Cefdinir with PVP K-30 and PEG 4000

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2010.3.2.8 ◽

2010 ◽

Vol 3 (2) ◽

pp. 948-956

Author(s):

Kumar P ◽

S Kumar ◽

A Kumar ◽

M Chander

Keyword(s):

Solid Dispersions ◽

Physicochemical Characterization ◽

Drug Carriers ◽

Dissolution Properties ◽

Rate Of Dissolution ◽

Peg 4000 ◽

Release Studies ◽

Crystalline Nature ◽

Physical Mixtures

The purpose of this study was to prepare and characterize solid dispersions of the antibacterial agent Cefdinir with PEG 4000 and PVP K-30 with a view to improve its dissolution properties. Investigations of the properties of the dispersions were performed using release studies, X-ray powder diffraction (XRD) and Fourier transform infrared (FTIR). The results obtained showed that the rate of dissolution of Cefdinir was considerably improved when formulated in solid dispersions with PVP K-30 and PEG 4000 as compared with pure drug and physical mixtures. The results from XRD studies showed the transition of crystalline nature of drug to amorphous form, while FTIR studies demonstrated the absence of drug-carriers interaction.

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Influence of the Preparation Method on the Dissolution Properties of Piroxicam - Cyclodextrins Systems

Letters in Drug Design & Discovery ◽

10.2174/1570180811666140207215957 ◽

2014 ◽

Vol 11 (6) ◽

pp. 786-808 ◽

Cited By ~ 2

Author(s):

F. Bouchal ◽

M. Skiba ◽

S. Fatmi ◽

N. Chaffai ◽

M. Lahiani-Skiba

Keyword(s):

Preparation Method ◽

Dissolution Properties

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Enhanced Dissolution of Naproxen by Combining Cocrystallization and Eutectic Formation

Pharmaceutics ◽

10.3390/pharmaceutics13050618 ◽

2021 ◽

Vol 13 (5) ◽

pp. 618

Author(s):

Hakyeong Kim ◽

Soeun Jang ◽

Il Won Kim

Keyword(s):

Model System ◽

Dissolution Behavior ◽

Active Pharmaceutical Ingredients ◽

Biorelevant Media ◽

Biologically Relevant ◽

Pharmaceutical Ingredients ◽

Enhanced Dissolution ◽

Dissolution Properties ◽

Eutectic Formation ◽

Combined Strategy

Improving dissolution properties of active pharmaceutical ingredients (APIs) is a critical step in drug development with the increasing occurrence of sparingly soluble APIs. Cocrystal formation is one of the methods to alter the physicochemical properties of APIs, but its dissolution behavior in biorelevant media has been scrutinized only in recent years. We investigated the combined strategy of cocrystallization and eutectic formation in this regard and utilized the cocrystal model system of naproxen and three pyridinecarboxamide isomers. Binary melting diagrams were constructed to discover the eutectic compositions of the three cocrystals with excess amounts of pyridinecarboxamides. The melt–crystallized eutectics and cocrystals were compared in their dissolution behaviors with respect to neat naproxen. The eutectics enhanced the early dissolution rates of the cocrystals in both the absence and presence of biologically relevant bile salt and phospholipid components, whereas the cocrystal dissolution was expedited and delayed, respectively. The combined strategy in the present study will be advantageous in maximizing the utility of the pharmaceutical cocrystals.

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Solubilization of Trans-Resveratrol in Some Mono-Solvents and Various Propylene Glycol + Water Mixtures

Molecules ◽

10.3390/molecules26113091 ◽

2021 ◽

Vol 26 (11) ◽

pp. 3091

Author(s):

Mohammed Ghazwani ◽

Prawez Alam ◽

Mohammed H. Alqarni ◽

Hasan S. Yusufoglu ◽

Faiyaz Shakeel

Keyword(s):

Propylene Glycol ◽

Mole Fraction ◽

Bioactive Compound ◽

Theoretical Models ◽

Solubility Parameters ◽

Hansen Solubility Parameters ◽

Neat Water ◽

Dissolution Properties ◽

Hansen Solubility

This research deals with the determination of solubility, Hansen solubility parameters, dissolution properties, enthalpy–entropy compensation, and computational modeling of a naturally-derived bioactive compound trans-resveratrol (TRV) in water, methanol, ethanol, n-propanol, n-butanol, propylene glycol (PG), and various PG + water mixtures. The solubility of TRV in six different mono-solvents and various PG + water mixtures was determined at 298.2–318.2 K and 0.1 MPa. The measured experimental solubility values of TRV were regressed using six different computational/theoretical models, including van’t Hoff, Apelblat, Buchowski–Ksiazczak λh, Yalkowsly–Roseman, Jouyban–Acree, and van’t Hoff–Jouyban–Acree models, with average uncertainties of less than 3.0%. The maxima of TRV solubility in mole fraction was obtained in neat PG (2.62 × 10−2) at 318.2 K. However, the minima of TRV solubility in the mole fraction was recorded in neat water (3.12 × 10−6) at 298.2 K. Thermodynamic calculation of TRV dissolution properties suggested an endothermic and entropy-driven dissolution of TRV in all studied mono-solvents and various PG + water mixtures. Solvation behavior evaluation indicated an enthalpy-driven mechanism as the main mechanism for TRV solvation. Based on these data and observations, PG has been chosen as the best mono-solvent for TRV solubilization.

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Correlation and prediction of solubility of hydrogen in alkenes and its dissolution properties

Applied Petrochemical Research ◽

10.1007/s13203-020-00260-w ◽

2021 ◽

Author(s):

Mohammad Jamali ◽

Amir Abbas Izadpanah ◽

Masoud Mofarahi

Keyword(s):

Equation Of State ◽

Binary Interaction ◽

Absolute Deviation ◽

Dissolution Properties ◽

Different Temperatures ◽

Binary Interaction Parameters ◽

Delta G ◽

Hoff Equation ◽

Increasing Temperature ◽

Total Average

AbstractIn this work, solubility of hydrogen in some alkenes was investigated at different temperatures and pressures. Solubility values were calculated using the Peng–Robinson equation of state. Binary interaction parameters were calculated using fitting the equation of state on experimental data, Group contribution method and Moysan correlations and total average absolute deviation for these methods was 3.90, 17.60 and 13.62, respectively. Because hydrogen solubility in Alkenes is low, Henry’s law for these solutions were investigated, too. Results of calculation showed with increasing temperature, Henry’s constant was decreased. The temperature dependency of Henry’s constants of hydrogen in ethylene and propylene was higher than to other alkenes. In addition, using Van’t Hoff equation, the thermodynamic parameters for dissolution of hydrogen in various alkenes were calculated. Results indicated that the dissolution of hydrogen was spontaneous and endothermic. The total average of dissolution enthalpy ($${\Delta H}^{^\circ }$$ Δ H ∘ ) and Gibbs free energy ($${\Delta G}^{^\circ }$$ Δ G ∘ ) for these systems was 3.867 kJ/mol and 6.361 kJ/mol, respectively. But dissolution of hydrogen in almost of alkenes was not an entropy-driven process.

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